+

WO2017038455A1 - Comprimé à désagrégation ultra-rapide et procédé pour le produire - Google Patents

Comprimé à désagrégation ultra-rapide et procédé pour le produire Download PDF

Info

Publication number
WO2017038455A1
WO2017038455A1 PCT/JP2016/073917 JP2016073917W WO2017038455A1 WO 2017038455 A1 WO2017038455 A1 WO 2017038455A1 JP 2016073917 W JP2016073917 W JP 2016073917W WO 2017038455 A1 WO2017038455 A1 WO 2017038455A1
Authority
WO
WIPO (PCT)
Prior art keywords
tablet
disintegrating
disintegrating tablet
particle composition
orally disintegrating
Prior art date
Application number
PCT/JP2016/073917
Other languages
English (en)
Japanese (ja)
Inventor
智仁 岡林
淳弘 上友
尚弘 橋川
隆弘 平邑
森田　哲郎
君子 池田
Original Assignee
株式会社ダイセル
ニチリン化学工業株式会社
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 株式会社ダイセル, ニチリン化学工業株式会社 filed Critical 株式会社ダイセル
Priority to KR1020187007654A priority Critical patent/KR20180041217A/ko
Priority to US15/754,492 priority patent/US10864165B2/en
Priority to JP2017537720A priority patent/JP6469234B2/ja
Priority to EP16841487.8A priority patent/EP3345626A4/fr
Priority to CN201680051003.5A priority patent/CN108136035A/zh
Publication of WO2017038455A1 publication Critical patent/WO2017038455A1/fr

Links

Images

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms

Definitions

  • the present invention relates to an orally disintegrating tablet which is a tablet having a large weight and is relatively thin and has an extremely short disintegration time in the oral cavity and / or a disintegration time in water, and a production method thereof.
  • Orally disintegrating tablets have been developed as highly convenient dosage forms that can be safely taken by patients, elderly people, children, etc. who have difficulty swallowing drugs, and can be easily taken without water.
  • Orally disintegrating tablets have sufficient breaking strength (tablet hardness) that does not cause chipping or pulverization of tablets during tablet production, transportation or opening, as with normal tablets, and promptly in the oral cavity. It is important to have an excellent disintegration property (disintegration time) that disintegrates.
  • tablet hardness and disintegration are properties that are opposite to each other.
  • increasing the molding pressure to increase the hardness increases the disintegration time
  • decreasing the molding pressure to decrease the disintegration time tends to decrease the hardness.
  • various techniques have been developed to achieve a balance between these two properties, or to achieve an optimal balance between the two properties.
  • particle components, granulation methods, and the like have been studied in order to impart excellent moldability to the particles or particle composition constituting the tablet.
  • Orally disintegrating tablets are known to improve patient compliance, but patients who have a strong tendency to refuse to take drugs are known to exhale tablets with an orally disintegrating time of about 20-30 seconds. It has been. Therefore, for example, if the disintegration time is about several seconds, if the disintegration is remarkably high, the tablet disintegrates before taking it uncomfortable at the time of taking the medicine.
  • Zydis (registered trademark) technology is known as a manufacturing technology for such a tablet having extremely high disintegration property in the oral cavity, that is, “ultra-fast disintegrating tablet”.
  • This is a manufacturing technique of an oral solid dosage form developed by Cardinal Health Co. (currently Catalant USA), as described in Patent Document 1, using gelatin as a carrier material,
  • This is a method for preparing a rapidly dispersible solid oral dosage form by suspending a bulk powder (medicinal component) together with mannitol and the like and then filling it into a blister, followed by lyophilization.
  • Patent Document 2 describes an invention relating to a method for producing a freeze-dried fast dissolving multiphase dosage form.
  • the method is a multi-phase rapid delivery method for delivering a pharmaceutically active ingredient by sequentially loading a formulation containing a non-gelling matrix-forming agent and a formulation containing a gelling matrix and lyophilizing them.
  • Solvent form (FDDF) is prepared.
  • Non-gelling gelatin is used as the non-gelling matrix forming agent
  • gelling gelatin is used as the gelling matrix forming agent.
  • Patent Document 3 describes an orally disintegrating tablet having a disintegration time in water of less than 15 seconds and a tablet hardness of 10 N or more.
  • the specific surface area of the tablet is substantially 0.75 to 1.50 mm. 2 / mg.
  • Patent Documents 4 to 7 describe various orally disintegrating tablets, but their specific surface areas are substantially in the range of 0.75 to 1.50 mm 2 / mg.
  • the above-described conventional technique requires a special device for performing freeze-drying, and cannot use a tableting machine with high production efficiency as in the case of producing ordinary tablets.
  • the ultra-fast disintegrating tablet produced by the prior art has extremely low tablet hardness, an ultra-fast disintegrating tablet that exhibits tablet hardness at a level that enables normal PTP packaging is desired.
  • the problem to be solved by the present invention is to solve the technical problems found in such conventional super-fast disintegrating tablets and to have a very high disintegration property (short disintegration time) capable of delivering a reliable patient's medication.
  • the present inventor has obtained a super fast disintegrating tablet which is a relatively thin tablet having a large weight and a very high disintegration property by setting physical properties such as the weight and specific surface area of the orally disintegrating tablet within a specific range. It discovered that it could manufacture using the conventional granulation process, and completed this invention.
  • the present invention provides the following aspects.
  • a disintegrating particle composition comprising a first disintegrant component comprising acid-type carboxymethylcellulose, which is used in the method for producing an orally disintegrating tablet according to any one of Embodiments 7 to 10.
  • a disintegrating particle composition according to aspect 11 further comprising crystalline cellulose.
  • an ultra-fast disintegrating tablet that is large and relatively thin and exhibits a very short oral disintegration time and / or disintegration time in water can be easily produced using a device similar to a normal tablet. it can.
  • the orally disintegrating tablet of the present invention has a specific surface area of about 1.50 to 4.00 mm 2 / mg, preferably about 1.50 to 3.50 mm 2 / mg, and a weight of about 100 to 300 mg, preferably about 100 to 200 mg.
  • Specific surface area is “surface area / tablet weight”.
  • the surface area can be determined by a commonly used general method. For example, in the case of a flat tablet, assuming that it is a cylinder, the surface area can be calculated by calculating the sum of the upper and lower circular parts and the side surface (surface area of the cylinder). Can be obtained.
  • the dosage form of the present invention is not particularly limited, and may be any shape known to those skilled in the art (for example, true flat tablet, standard R surface, sugar-coated R surface, rounded round tablet (flat), rounded flat tablet (flat) and Can take a two-step rounded surface.
  • the diameter of the tablet can be set as appropriate, but is usually about 12 mm or more, for example, about 12 mm to 18 mm.
  • the tablet thickness is usually about 0.50 mm to 1.80 mm, which is a relatively thin tablet.
  • the tablet hardness needs to be high to some extent, and is usually about 5N or more, preferably about 5N to 30N, more preferably about 5N to 21N.
  • the disintegration time in water is about 7 seconds or less, preferably 5 seconds or less
  • the oral disintegration time is 6 seconds or less, preferably 5 seconds or less. This satisfies the demand sufficiently.
  • the medicinal ingredient contained in the orally disintegrating tablet of the present invention is a nutritional ingredient in a pharmaceutical ingredient, food or health food.
  • a medicinal component alone or a component obtained by coating or granulating the medicinal component for the purpose of slow release or bitterness masking can be added.
  • the medicinal component contained in the orally disintegrating tablet of the present invention there are no particular restrictions on the use and type of the medicinal component contained in the orally disintegrating tablet of the present invention.
  • the use and type of the medicinal component include those for central nervous system, drugs for peripheral nervous system, and sensory organs. Medicine, vaginal cardiovascular medicine, respiratory organ medicine, digestive organ medicine, hormone agent, urogenital organ medicine, other individual organ system medicines, vitamins, nourishing tonics, blood and body fluid medicines, other metabolic properties Pharmaceuticals, sputum cell-stimulating drugs, oncology drugs, radiopharmaceuticals, allergy drugs, other tissue cell functional drugs, vaginal drugs, Kampo medicines, other herbal medicines and medicines based on Kampo medicines, antibiotics, chemotherapeutics, biological Pharmacological preparations, drugs for parasites, drugs for other pathogenic organisms, preparation drugs, diagnostic drugs, public health drugs, in vitro diagnostic drugs, and the like.
  • the orally disintegrating tablet of the present invention includes, in addition to medicinal ingredients, excipients, surfactants, lubricants, sour agents, sweeteners, corrigents, fragrances, colorants, stabilizers and the like as necessary. Any other pharmaceutically acceptable ingredient may be included.
  • any other pharmaceutically acceptable ingredient may be included.
  • light anhydrous silicic acid and / or ⁇ -cyclodextrin can be added for the purpose of improving fluidity and imparting sweetness.
  • these optional components for example, the corresponding components described in the Pharmaceutical Additives Dictionary (Pharmaceutical Daily) and the Japanese Pharmacopoeia can be used.
  • a disintegrating particle composition is mixed with a medicinal component (or a pharmaceutical composition containing the medicinal component) and other optional components described above, and the resulting mixture is obtained, for example, in the present specification.
  • a suitable tableting machine known to those skilled in the art as described in the examples in the description, for example, with a tableting compression force of about 2 to 20 kN, preferably about 5 to 20 kN.
  • a manufacturing method can be mentioned.
  • a method called an “external lubricant tableting method” in which a lubricant such as magnesium stearate is previously sprayed or applied to a mortar and pestle of a tableting machine for lubrication can be used. Therefore, the present invention also relates to a collapsible particle composition used in such a production method.
  • the form (state) of the medicinal component and the like for example, it may be in a powder state.
  • mixing (solid trituration) and tableting of medicinal ingredients and the disintegrating particle composition can be carried out by any means / method known to those skilled in the art. At this time, the amount of the active ingredient contained in the orally disintegrating tablet can be easily adjusted so as to obtain an appropriate dosage according to the administration subject and administration purpose.
  • Wicking is a disintegration mechanism in which moisture penetrates through components such as a disintegrant contained in a tablet, and as a result, the binding force between particles contained in the tablet weakens and proceeds.
  • Acid type carboxymethyl cellulose is known as a representative example of such a disintegrant having a high effect of promoting wicking.
  • Swelling is a disintegration mechanism in which the disintegrant itself swells and proceeds as a result of water permeating into the disintegrant.
  • the disintegrating particle composition of the present invention preferably contains acid carboxymethylcellulose as the first disintegrant component.
  • the acid-type carboxymethyl cellulose is a substance called carmellose and is used as a pharmaceutical additive. Similar to acid-type carboxymethylcellulose, for example, calcium salt of carboxymethylcellulose and a crosslinked product of sodium carboxymethylcellulose are both insoluble in water and used as a disintegrant in tablets and the like. On the other hand, sodium salt of carboxymethyl cellulose is water-soluble and is used for the purpose of a binder or the like. In addition, the salt of carboxymethylcellulose may be described as carmellose.
  • any disintegrating agent known to those skilled in the art other than acid-type carboxymethylcellulose can be used as the second disintegrating agent component of the disintegrating particle composition of the present invention.
  • a disintegrant excellent in the effect of promoting swelling as a second disintegrant component other than Wicking, for example.
  • disintegrants include crospovidone, croscarmellose sodium, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, carboxymethyl cellulose calcium, hydroxypropyl starch, and starch.
  • Crospovidone is a common name for a crosslinked polymer of 1-vinyl-2-pyrrolidone
  • croscarmellose sodium is a common name for a crosslinked product of sodium carboxymethylcellulose.
  • crospovidone croscarmellose sodium, carboxymethyl starch sodium, low-substituted hydroxypropylcellulose, or any combination of two or more selected from carboxymethylcellulose calcium is preferable.
  • any compound known to those skilled in the art as an excipient is included.
  • Representative examples thereof include sugars or sugar alcohols such as mannitol, erythritol, sorbitol, D-glutitol (maltitol), xylitol, trehalose, lactose and maltose.
  • preferred examples include mannitol, erythritol, trehalose, sorbitol, and D-glutitol (maltitol).
  • two or more compounds appropriately selected from these can be used.
  • the disintegrating particle composition preferably contains crystalline cellulose known to those skilled in the art.
  • Representative examples thereof include commercially available products such as Avicel (FMC Corporation), Theolas (Asahi Kasei Chemicals), and Viva Poor (Lettemeyer).
  • disintegrating particle composition of the present invention is appropriately mixed with various optional components known to those skilled in the art for the purpose of adjusting various properties such as disintegration force, binding force, and tablet feeling. May be.
  • optional components include fluidizers, sweeteners, fragrances, and colorants.
  • the amount of each component in the disintegrating particle composition of the present invention depends on the type of each component, the type and use of the medicinal component that is the target of use of the disintegrating particle composition, the use of the orally disintegrating tablet that is the final product, etc. Thus, those skilled in the art can appropriately determine.
  • the first disintegrant component is in the range of 10 to 50% by weight
  • the second disintegrant component is in the range of 1 to 20% by weight
  • the excipient is in the range of 30 to 88% by weight, based on the total weight of the disintegrating particle composition.
  • the crystalline cellulose is in the range of 1 to 40% by weight.
  • the disintegrating particle composition of the present invention can be produced by any method known to those skilled in the art. For example, a first wet granulation step using any one or two components, a two-stage granulation step comprising a second wet granulation step using at least the granulated product obtained in the first wet granulation step and the remaining components It can be manufactured by a three-stage granulation step including a third step of further mixing components in the step or the granulated product obtained in the second wet granulation step.
  • the collapsible particle composition of the present invention may be produced by a one-step granulation process using all the components together.
  • each granulation step is performed by a method of forming a composite by dispersing and drying each component in the presence of water, that is, a wet granulation method.
  • a wet granulation method include spraying methods such as spray drying, tumbling granulation, stirring granulation, and fluidized bed granulation, freeze-drying methods, and kneading granulation. It can be produced by any method known to those skilled in the art.
  • disintegrants such as acid-type carboxymethylcellulose are hydrophilic
  • by performing an operation of applying physical force such as stirring in the presence of water by wet granulation particles from the aggregated state at the time of dry powder becomes more dispersed.
  • Fluidized bed granulation for dispersion and drying by water spray, spray drying, tumbling granulation, stirring granulation, etc. can be performed most easily and the drying speed is fast, so these methods are preferable. .
  • the fluidized bed granulation method is a granulation method performed by spraying water or an aqueous solution containing a binder while blowing up the powder with warm air, and it is easy to adjust the spraying conditions and the like. Is the most preferred method.
  • each granulation step various conditions such as spraying speed, air supply temperature, exhaust temperature, air supply amount, etc. can be appropriately determined by those skilled in the art according to the type and amount of each component. .
  • examples of the spray liquid medium include solvents acceptable for pharmaceuticals and foods such as water, ethanol, methanol, and acetone.
  • examples of the spray liquid include an aqueous solution in which less than 10% of the components of the collapsible particle composition are dissolved, and water or the aqueous solution is particularly preferable.
  • said disintegrating particle composition has the following physical properties. (1) Average particle size: 50 to 200 microns, (2) Water content: 0.5 to 6% by weight.
  • Average particle size 2 g of disintegrating particle composition is measured using a ⁇ 75 mm automatic shaking sieve (M-2 type, Tsutsui Riken Kikai Co., Ltd.).
  • Moisture 5 g of disintegrating particle composition is measured using a halogen moisture meter (HB43 type, METTLER TOLEDO).
  • the granulated product had the following physical property values. (1) Average particle size: 93 microns, (2) Water content: 2.3% by weight.
  • Example 1 for Orally Disintegrating Tablets
  • 0.51 part by weight of magnesium stearate was mixed with 99.5 parts by weight of the disintegrating particle composition obtained in Example 1 [Production of disintegrating particle composition], and a hand press tableting machine (HANDTAB-100, Ichihashi) was mixed. Seiki Co., Ltd.) was used for tableting at a tableting compression force of 18 kN to obtain a tablet having a diameter of 14.0 mm, a thickness of 0.80 mm, a true flat tablet, and a weight of 150 mg.
  • Example 9 [Production Example 2 for Orally Disintegrating Tablets] 99.5 parts by weight of the disintegrating particle composition obtained was mixed with 0.5 parts by weight of magnesium stearate and compressed using a hand press tableting machine. Tableting was performed at a force of 18 kN to obtain a tablet having a diameter of 14.0 mm, a thickness of 1.07 mm, a straight tablet, and a weight of 200 mg.
  • Example 3 for Orally Disintegrating Tablets
  • 99.8 parts by weight of the disintegrating particle composition was mixed with 0.2 part by weight of magnesium stearate, and compressed using a hand press tableting machine. Tableting was performed at a force of 8 kN to obtain a tablet having a diameter of 14.0 mm, a thickness of 1.51 mm, a true flat tablet, and a weight of 250 mg.
  • Example 4 for Orally Disintegrating Tablets
  • 99.8 parts by weight of the disintegrating particle composition was mixed with 0.2 part by weight of magnesium stearate, and compressed using a hand press tableting machine. Tableting was performed at a force of 18 kN to obtain a tablet having a diameter of 14.0 mm, a thickness of 0.55 mm, a straight tablet, and a weight of 100 mg.
  • Example 1 [Production Example 5 for Orally Disintegrating Tablets]
  • Example 1 [Production of disintegrating particle composition] 88.5 parts by weight of the disintegrating particle composition 10.0 parts by weight of ascorbic acid, 1.0 part by weight of light anhydrous silicic acid, 0. 5 parts by weight was mixed, and tableting was performed using a rotary tablet machine (HT-EX12SS-U, Hata Seiko Co., Ltd.) at a tableting compression force of 18 kN, diameter 14.0 mm, thickness 0.78 mm, true flat tablet A tablet with a weight of 150 mg was obtained.
  • a rotary tablet machine H-EX12SS-U, Hata Seiko Co., Ltd.
  • a hand press was prepared by mixing 95.3 parts by weight of the disintegrating particle composition obtained in Example 1 [Production of disintegrating particle composition] with 4.2 parts by weight of crospovidone XL and 0.5 parts by weight of magnesium stearate. Tableting was performed using a tableting machine at a tableting compression force of 18 kN to obtain a tablet having a diameter of 14.0 mm, a thickness of 0.81 mm, a true tablet, and a weight of 150 mg.
  • Example 8 for Orally Disintegrating Tablets 19.5 parts by weight of carmellose and 0.5 parts by weight of magnesium stearate were mixed with 89.5 parts by weight of the disintegratable particle composition obtained in Example 1 [Production of disintegrating particle composition], and hand-press tableting was performed.
  • the tablet was compressed at a compression force of 18 kN using a machine to obtain a tablet having a diameter of 14.0 mm, a thickness of 0.80 mm, a true flat tablet, and a weight of 150 mg.
  • Example 9 Manufacture of disintegrating particle composition
  • 97.5 parts by weight of the disintegrating particle composition was mixed with 2.0 parts by weight of croscarmellose sodium and 0.5 part by weight of magnesium stearate to prepare a hand. Tableting was performed using a press tableting machine at a tableting compression force of 18 kN to obtain a tablet having a diameter of 14.0 mm, a thickness of 0.81 mm, a true tablet, and a weight of 150 mg.
  • a hand press was prepared by mixing 10.0 parts by weight of L-HPC and 0.5 parts by weight of magnesium stearate with 89.5 parts by weight of the disintegrating particle composition obtained in Example 1 [Production of disintegrating particle composition]. Tableting was performed using a tableting machine at a tableting compression force of 18 kN to obtain a tablet having a diameter of 14.0 mm, a thickness of 0.81 mm, a true tablet, and a weight of 150 mg.
  • Example 1 [Manufacture of orally disintegrating tablets 11]
  • Example 1 [Production of disintegrating particle composition] 69.7 parts by weight of the disintegrating particle composition, 30.0 parts by weight of etenzaamide, 1.0 part by weight of light anhydrous silicic acid, 0.3 mg of magnesium stearate The weight parts were mixed, and tableting was performed using a rotary tablet machine (HT-EX12SS-U, Hata Seiko Co., Ltd.) at a tableting compression force of 18 kN, diameter 14.0 mm, thickness 0.80 mm, straight tablets, A tablet weighing 150 mg was obtained.
  • a rotary tablet machine HT-EX12SS-U, Hata Seiko Co., Ltd.
  • Example 1 [Manufacture of orally disintegrating tablets 12]
  • Example 1 [Manufacture of disintegrating particle composition] 88.3 parts by weight of the disintegrating particle composition 10.0 parts by weight of acetaminophen, 1.0 part by weight of light anhydrous silicic acid, magnesium stearate 0 .7 parts by weight were mixed, and tableting was performed using a rotary tableting machine (HT-EX12SS-U, Hata Seiko Co., Ltd.) at a tableting compression force of 18 kN, diameter 14.0 mm, thickness 0.82 mm, Shinpei A tablet having a weight of 150 mg was obtained.
  • a rotary tableting machine HT-EX12SS-U, Hata Seiko Co., Ltd.
  • Hardness Hardness (N) was measured using a digital Kiya-type hardness meter (Fujiwara Manufacturing Co., Ltd.).
  • Disintegration time in water The disintegration time in water was measured using a disintegration tester (NT-400, Toyama Sangyo Co., Ltd.) according to the method described in the Japanese Pharmacopoeia (but without an auxiliary board).
  • Oral disintegration time Oral disintegration time was measured using an oral disintegration tester (Trichop Tester, Okada Seiko Co., Ltd.).
  • Table 1 shows various physical property values of the tablets (Examples 2 to 13) of the present invention thus produced.
  • the present invention not only can patients who have difficulty swallowing drugs, elderly people, children, etc. be able to take safely and easily without water, but also have a strong tendency to refuse medication.
  • Highly disintegratable (short disintegration time) that can be used for drug administration, and has a tablet hardness that is expected to reduce chipping of tablets to a practical level. It becomes possible to provide an orally disintegrating tablet (super-fast disintegrating tablet).

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Zoology (AREA)
  • Inorganic Chemistry (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne : un comprimé à désintégration orale (comprimé à désintégration ultra-rapide), qui a un poids important et une épaisseur relativement petite et présente une propriété de désintégration extrêmement élevée (une courte durée de désintégration); et un procédé simple pour produire le comprimé à désintégration ultra-rapide sans qu'il soit nécessaire d'effectuer une lyophilisation qui est une opération complexe. La présente invention concerne : un comprimé à désagrégation orale ayant une surface spécifique de 1,50 à 4,00 mm2/mg et un poids de 100 à 300 mg, et en particulier, qui présente une durée de désagrégation dans l'eau de 7 secondes ou moins et une durée de désagrégation dans la cavité orale de 6 secondes ou moins; un procédé de production du comprimé à désagrégation orale; et une composition de particules se désagrégeant qui est utilisée dans le procédé de production.
PCT/JP2016/073917 2015-09-04 2016-08-16 Comprimé à désagrégation ultra-rapide et procédé pour le produire WO2017038455A1 (fr)

Priority Applications (5)

Application Number Priority Date Filing Date Title
KR1020187007654A KR20180041217A (ko) 2015-09-04 2016-08-16 초고속 붕해 정제 및 그 제조 방법
US15/754,492 US10864165B2 (en) 2015-09-04 2016-08-16 Super-rapid disintegrating tablet, and method for producing same
JP2017537720A JP6469234B2 (ja) 2015-09-04 2016-08-16 超速崩壊錠剤及びその製造方法
EP16841487.8A EP3345626A4 (fr) 2015-09-04 2016-08-16 Comprimé à désagrégation ultra-rapide et procédé pour le produire
CN201680051003.5A CN108136035A (zh) 2015-09-04 2016-08-16 超速崩解片剂及其制备方法

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2015174953 2015-09-04
JP2015-174953 2015-09-04

Publications (1)

Publication Number Publication Date
WO2017038455A1 true WO2017038455A1 (fr) 2017-03-09

Family

ID=58188584

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2016/073917 WO2017038455A1 (fr) 2015-09-04 2016-08-16 Comprimé à désagrégation ultra-rapide et procédé pour le produire

Country Status (7)

Country Link
US (1) US10864165B2 (fr)
EP (1) EP3345626A4 (fr)
JP (1) JP6469234B2 (fr)
KR (1) KR20180041217A (fr)
CN (1) CN108136035A (fr)
TW (2) TWI762450B (fr)
WO (1) WO2017038455A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020027247A1 (fr) 2018-08-03 2020-02-06 株式会社ダイセル Tablette mince, méthode de fabrication de tablette mince, et dispositif de fabrication de tablette mince
WO2020036105A1 (fr) 2018-08-17 2020-02-20 株式会社ダイセル Corps d'emballage, corps d'emballage avec comprimé, procédé de fabrication d'élément d'accueil de corps d'emballage, et appareil de fabrication d'élément d'accueil de corps d'emballage

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116008490B (zh) * 2022-11-30 2025-04-29 浙江大学 一种可模拟口腔环境的口崩片崩解测定装置及测定方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014096669A1 (fr) * 2012-12-17 2014-06-26 Ethypharm Comprimes orodispersibles obtenus par compression moulage
WO2015005241A1 (fr) * 2013-07-06 2015-01-15 株式会社ダイセル Comprimé à désagrégration ultrarapide et sa méthode de fabrication
JP2015078182A (ja) * 2013-09-14 2015-04-23 富士化学工業株式会社 速崩壊性圧縮成型物及びその製法
JP2015134838A (ja) * 2015-05-07 2015-07-27 ニプロ株式会社 口腔内崩壊剤及びその製造方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1736144E (pt) * 1998-05-18 2016-02-10 Takeda Pharmaceutical Comprimidos de desintegração oral
WO2002030400A1 (fr) * 2000-10-06 2002-04-18 Takeda Chemical Industries, Ltd. Preparations solides
ES2199061B1 (es) * 2002-06-10 2005-02-16 Laboratorios Vita, S.A. Comprimidos bucodispersables y procedimiento para su obtencion.
EP2101738A2 (fr) 2006-12-21 2009-09-23 Mallinckrodt Inc. Comprimés à désintégration par voie orale: composition utilisée et méthode de fabrication orale
WO2008081891A1 (fr) * 2006-12-28 2008-07-10 Takeda Pharmaceutical Company Limited Préparation solide se désintégrant oralement
WO2009066773A1 (fr) * 2007-11-21 2009-05-28 Dainippon Sumitomo Pharma Co., Ltd. Comprimé se désintégrant oralement
JP2016117652A (ja) * 2013-04-16 2016-06-30 株式会社ダイセル 小児への投与に適した速崩壊錠とその簡便な製造方法

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014096669A1 (fr) * 2012-12-17 2014-06-26 Ethypharm Comprimes orodispersibles obtenus par compression moulage
WO2015005241A1 (fr) * 2013-07-06 2015-01-15 株式会社ダイセル Comprimé à désagrégration ultrarapide et sa méthode de fabrication
JP2015078182A (ja) * 2013-09-14 2015-04-23 富士化学工業株式会社 速崩壊性圧縮成型物及びその製法
JP2015134838A (ja) * 2015-05-07 2015-07-27 ニプロ株式会社 口腔内崩壊剤及びその製造方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of EP3345626A4 *

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020027247A1 (fr) 2018-08-03 2020-02-06 株式会社ダイセル Tablette mince, méthode de fabrication de tablette mince, et dispositif de fabrication de tablette mince
JP2020019750A (ja) * 2018-08-03 2020-02-06 株式会社ダイセル 薄型錠剤、薄型錠剤製造方法、及び薄型錠剤製造装置
KR20210041022A (ko) 2018-08-03 2021-04-14 주식회사 다이셀 박형 정제, 박형 정제 제조방법, 및 박형 정제 제조장치
WO2020036105A1 (fr) 2018-08-17 2020-02-20 株式会社ダイセル Corps d'emballage, corps d'emballage avec comprimé, procédé de fabrication d'élément d'accueil de corps d'emballage, et appareil de fabrication d'élément d'accueil de corps d'emballage
KR20210044842A (ko) 2018-08-17 2021-04-23 주식회사 다이셀 포장체, 정제가 들어 있는 포장체, 포장체의 수용 부재의 제조방법, 및 포장체의 수용 부재의 제조장치
EP3838794A4 (fr) * 2018-08-17 2022-05-04 Daicel Corporation Corps d'emballage, corps d'emballage avec comprimé, procédé de fabrication d'élément d'accueil de corps d'emballage, et appareil de fabrication d'élément d'accueil de corps d'emballage
US12128005B2 (en) 2018-08-17 2024-10-29 Daicel Corporation Packaging body, tablet-containing packaging body, method for manufacturing accommodation member of packaging body, and apparatus for manufacturing accommodation member of packaging body

Also Published As

Publication number Publication date
KR20180041217A (ko) 2018-04-23
CN108136035A (zh) 2018-06-08
JPWO2017038455A1 (ja) 2018-06-14
EP3345626A1 (fr) 2018-07-11
JP6469234B2 (ja) 2019-02-13
US10864165B2 (en) 2020-12-15
US20180235889A1 (en) 2018-08-23
TW202211909A (zh) 2022-04-01
TWI762450B (zh) 2022-05-01
TW201717916A (zh) 2017-06-01
EP3345626A4 (fr) 2019-07-24

Similar Documents

Publication Publication Date Title
US20060240101A1 (en) Orally disintegrating pharmaceutical tablet formulations of olanzapine
JP2019131597A (ja) 超速崩壊錠剤及びその製造方法
JP6479658B2 (ja) 超速崩壊錠剤及びその製造方法
TW201726113A (zh) 易服用性固態製劑用粒子組成物及含有該粒子組成物之易服用性固態製劑
JP6469234B2 (ja) 超速崩壊錠剤及びその製造方法
JP3884056B1 (ja) 口腔内速崩錠の製造方法
JP4601271B2 (ja) 圧縮成形製剤およびその製造方法
WO2014171307A1 (fr) Comprime a dissolution rapide approprie pour une administration a des nourrissons, et son procédé de production simple
JP6853191B2 (ja) 口腔内保持型崩壊性固形製剤、その製造方法、及び該製造方法に用いる粉体組成物
WO2016060035A1 (fr) Comprimé à désintégration ultra-rapide
TW201609193A (zh) 含有碳酸鹽之口腔內崩解錠劑用組成物及口腔內崩解錠劑

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 16841487

Country of ref document: EP

Kind code of ref document: A1

ENP Entry into the national phase

Ref document number: 2017537720

Country of ref document: JP

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 15754492

Country of ref document: US

NENP Non-entry into the national phase

Ref country code: DE

ENP Entry into the national phase

Ref document number: 20187007654

Country of ref document: KR

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 2016841487

Country of ref document: EP

点击 这是indexloc提供的php浏览器服务，不要输入任何密码和下载